| Cas No.: | 1362850-20-1 |
| Chemical Name: | Seletalisib |
| Synonyms: | Seletalisib;UCB5857;(R)-3-(8-chloro-3-(2,2,2-trifluoro-1-(pyrido[3,2-d]pyrimidin-4-ylamino)ethyl)quinolin-2-yl)pyridine 1-oxide;64CW205BDD;GTPL9800;BCP29404;UCB 5857;DB12706;A16797;Q27263741;3-{8-chloro-3-[(1R)-2,2,2-trifluoro-1-({pyrido[3,2-d]pyrimidin-4-yl}amino)ethyl]quinolin-2-yl}pyridin-1-ium-1-olate |
| SMILES: | ClC1=CC=CC2=C1N=C(C1=CC=C[N+](=C1)[O-])C(=C2)[C@H](C(F)(F)F)NC1C2C(=CC=CN=2)N=CN=1 |
| Formula: | C23H14ClF3N6O |
| M.Wt: | 482.845073223114 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Seletalisib is a potent, ATP-competitive and highly selective PI3Kδ inhibitor able to block AKT phosphorylation following activation of the BCR in a B-cell line. Seletalisib inhibits N-formyl peptides (fMLP)-stimulated but not phorbol myristate acetate (PMA)-stimulated superoxide release from human neutrophils consistent with a PI3Kδ-specific activity. No indications of cytotoxicity are observed in PBMCs or other cell types treated with seletalisib. seletalisib blocks human T-cell production of several cytokines from activated T-cells. Seletalisib inhibits T-cell differentiation to Th1, Th2, and Th17 subtypes. Additionally, seletalisib inhibits B-cell proliferation and cytokine release. In human whole blood assays, seletalisib inhibits CD69 expression upon B-cell activation and anti-IgE-mediated basophil degranulation.Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat. The inhibition is observed at all tested doses of seletalisib with almost complete inhibition reached at dose levels ≥1 mg/kg. Seletalisib has potent in vivo effects with an estimated IC50 value of <10 nM. |
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| 2018-0101 |
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